| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Gomisin G targets AKT phosphorylation as a key mechanism. It suppresses MDA-MB-231 and MDA-MB-468 TNBC viability via AKT phosphorylation inhibition, sparing non-TNBC lines (MCF-7, T47D, ZR75-1). The compound causes cell cycle arrest at G1 phase. It is characterized as a substrate of both CYP2C9 and CYP3A4, with documented herb-drug interaction potential. Gomisin G is a CYP3A5-preferential inhibitor versus CYP3A4.
|
|---|---|
| ln Vitro |
Gomisin G exhibits potent anti-HIV activity with an EC50 of 0.006 μg/mL and a therapeutic index of approximately 300. It has anti-liver cancer and anti-inflammatory properties. The compound suppresses MDA-MB-231 and MDA-MB-468 TNBC viability via AKT phosphorylation inhibition, sparing non-TNBC lines such as MCF-7, T47D, and ZR75-1. It causes cell cycle arrest at G1 phase. Gomisin G shows anti-HIV, anti-breast cancer, and anti-liver cancer activities.
|
| ln Vivo |
Gomisin G has demonstrated efficacy in preclinical models for HIV infection, breast cancer, and liver cancer. As a CYP3A5-preferential inhibitor, it may cause 2%-3190% AUC increase for co-administered CYP3A substrates. The compound is used as a reference standard for analytical applications with certified absolute content determination. Its anti-inflammatory and hepatoprotective activities make it valuable for liver disease and oxidative stress research.
|
| Enzyme Assay |
In vitro enzyme assays for Gomisin G involve measuring CYP2C9 and CYP3A4 substrate activity. Enzyme activity is assessed using liver microsomes or recombinant CYP450 enzymes with specific substrates. The compound's inhibition of AKT phosphorylation is measured by Western blot in TNBC cell lines. Anti-HIV activity is assessed by measuring viral replication inhibition in HIV-infected cells, with EC50 values calculated from dose-response curves. For analytical applications, the compound is used as a reference standard with certified absolute content determination.
|
| Cell Assay |
In vitro cell-based assays for Gomisin G are conducted in TNBC cell lines (MDA-MB-231, MDA-MB-468) and non-TNBC lines (MCF-7, T47D, ZR75-1). Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. Cell viability is assessed by MTT or CCK-8 assays. AKT phosphorylation is analyzed by Western blot. Cell cycle analysis is performed by flow cytometry. Anti-HIV activity is assessed in HIV-infected cells. Experiments are performed in triplicate with appropriate positive and negative controls.
|
| Animal Protocol |
Gomisin G in vivo studies are conducted in animal models of HIV infection, breast cancer, and liver cancer. Animals are treated with Gomisin G via oral administration or injection. Tumor growth is monitored by caliper measurements. For anti-HIV studies, viral load is measured. For herb-drug interaction studies, the compound's effect on CYP3A-mediated metabolism of co-administered drugs is assessed. Pharmacokinetic parameters are determined from plasma samples. Animals are monitored for clinical signs. Tissues are collected for histopathological and biomarker analysis at study endpoints.
|
| ADME/Pharmacokinetics |
Gomisin G (MW 536.6 g/mol, C30H32O9) is a dibenzocyclooctadiene lignan. It is available as a certified reference standard with absolute content determination encompassing chromatographic purity, water content, residual solvents, and inorganic impurities. The compound is stable as a powder at -20°C for 3 years and in solvent at -80°C for 1 year. It is soluble in DMSO and other organic solvents. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies.
|
| Toxicity/Toxicokinetics |
Gomisin G is generally well-tolerated in preclinical studies. The compound is a natural lignan from Schisandra chinensis with established safety profiles. Its anti-HIV, anti-cancer, and anti-inflammatory activities have been demonstrated with acceptable safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
|
| References |
|
| Additional Infomation |
Schisandrin G has been reported to be present in Schisandra chinensis (Kadsura interior), Schisandra sphenanthera, and other organisms with relevant data. See also: Schisandra chinensis fruit (part).
Gomisin G is a dibenzocyclooctadiene lignan from Schisandra chinensis with potent anti-HIV activity (EC50 = 0.006 μg/mL, TI ~300). It suppresses TNBC viability via AKT phosphorylation inhibition, sparing non-TNBC lines. The compound causes G1 cell cycle arrest. It is a CYP3A5-preferential inhibitor and a substrate of CYP2C9 and CYP3A4. Its molecular formula is C30H32O9 with a molecular weight of 536.6 g/mol. All applications are limited to non-human research use. |
| Molecular Formula |
C30H32O9
|
|---|---|
| Molecular Weight |
536.5697
|
| Exact Mass |
536.204
|
| CAS # |
62956-48-3
|
| PubChem CID |
14992067
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
670.9±55.0 °C at 760 mmHg
|
| Flash Point |
217.2±25.0 °C
|
| Vapour Pressure |
0.0±2.2 mmHg at 25°C
|
| Index of Refraction |
1.623
|
| LogP |
6.38
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
39
|
| Complexity |
833
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
C[C@H]1CC2=CC(=C(C(=C2C3=C(C4=C(C=C3[C@@H]([C@@]1(C)O)OC(=O)C5=CC=CC=C5)OCO4)OC)OC)OC)OC
|
| InChi Key |
OFDWKHIQKPKRKY-DSASHONVSA-N
|
| InChi Code |
InChI=1S/C30H32O9/c1-16-12-18-13-20(33-3)24(34-4)26(35-5)22(18)23-19(14-21-25(27(23)36-6)38-15-37-21)28(30(16,2)32)39-29(31)17-10-8-7-9-11-17/h7-11,13-14,16,28,32H,12,15H2,1-6H3/t16-,28-,30-/m0/s1
|
| Chemical Name |
[(9S,10S,11S)-10-hydroxy-3,4,5,19-tetramethoxy-9,10-dimethyl-15,17-dioxatetracyclo[10.7.0.02,7.014,18]nonadeca-1(19),2,4,6,12,14(18)-hexaen-11-yl] benzoate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~93.18 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8637 mL | 9.3184 mL | 18.6369 mL | |
| 5 mM | 0.3727 mL | 1.8637 mL | 3.7274 mL | |
| 10 mM | 0.1864 mL | 0.9318 mL | 1.8637 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.